Alectinib | Potent and selective ALK inhibitor
NMR (Conforms)
Available Options
| Size: | Price | Quantity | |
|---|---|---|---|
| 5 mg | $60.00 | ||
| 25 mg | $205.00 |
Alectinib (1256580-46-7) is a potent (IC50 = 1.9 nM) and highly selective ALK inhibitor.1 It blocked phosphorylation of both native ALK and the L1196M, C1156Y, and F1174L mutants. Alectinib has also been shown to inhibit RET kinase (IC50 = 4.8 nM), the RET gatekeeper mutations V804L and V804M, and inhibited the growth of RET fusion positive cells.2 Alectinib is clinically useful in the treatment of ALK-positive Non-Small Cell Lung Cancer. It effectively suppressed cell proliferation and induced apoptosis in a mouse neuroblastoma xenograft.3
References/Citations:
1) Sakamoto et al. (2011), CH5424802, a selective ALK inhibitor capable of blocking the resistant gatekeeper mutant; Cancer Cell, 19 679
2) Kodama et al. (2014), Alectinib Shows Potent Antitumor Activity against RET-Rearranged Non-Small Cell Lung Cancer., Mol. Cancer Ther. 13 2910
3) Lu et al. (2017), The second-generation ALK inhibitor alectinib effectively induces apoptosis in human neuroblastoma cells and inhibits tumor growth in a TH-MYCN transgenic neuroblastoma mouse model; Cancer Lett, 400 61
NMR (Conforms)
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Alectinib (1256580-46-7) is a potent (IC50 = 1.9 nM) and highly selective ALK inhibitor.1 It blocked phosphorylation of both native ALK and the L1196M, C1156Y, and F1174L mutants. Alectinib has also been shown to inhibit RET kinase (IC50 = 4.8 nM), the RET gatekeeper mutations V804L and V804M, and inhibited the growth of RET fusion positive cells.2 Alectinib is clinically useful in the treatment of ALK-positive Non-Small Cell Lung Cancer. It effectively suppressed cell proliferation and induced apoptosis in a mouse neuroblastoma xenograft.3
References/Citations:
1) Sakamoto et al. (2011), CH5424802, a selective ALK inhibitor capable of blocking the resistant gatekeeper mutant; Cancer Cell, 19 679
2) Kodama et al. (2014), Alectinib Shows Potent Antitumor Activity against RET-Rearranged Non-Small Cell Lung Cancer., Mol. Cancer Ther. 13 2910
3) Lu et al. (2017), The second-generation ALK inhibitor alectinib effectively induces apoptosis in human neuroblastoma cells and inhibits tumor growth in a TH-MYCN transgenic neuroblastoma mouse model; Cancer Lett, 400 61
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Focus Biomolecules • Plymouth Meeting, PA USA • 1-855-FOCUS21
Focus Biomolecules
Plymouth Meeting, PA USA
1-855-FOCUS21
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